Hepatotoxicity inducer, significantly up-regulating the expression of genes involved in endoplasmic reticulum stress and Toll-like receptor (TLR) pathway

Novel long-acting β 2 -adrenoceptor agonist

Novel potent BET protein degrader, inhibiting cell proliferation due to suppressed C-MYC transcription

Novel selective opioid receptor antagonist at all three receptor types

Novel IKZF1/3 degrader, inhibiting the proliferation of multiple myeloma cells in vitro as well as in vivo

Novel degrader of the anaplastic lymphoma kinase (ALK) fusion protein, effectively inducing ALK degradation and inhibiting the growth of ALK fusion positive cell lines, SU-DHL-1 and H3122, significantly reducing the tumor growth in H3122 xenograft model

Sorafenib analogue, retaining cytotoxicity similar to sorafenib in various human cancer cell lines and strongly inhibiting growth in the NCI-60 cell line panel

Potent equilibrative nucleoside transporter 4 (ENT4) inhibitor

Insulin receptor sensitizing agent; Selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B)

Novel GPR35 agonist

Novel potent and selective CHK1 kinase inhibitor

Potent and selective polo-like kinase 2 (PLK2) inhibitor

Nonpeptide partial agonist of oxytocin (OT) and vasopressin V2 receptors

Highly potent NR2B-selective NMDA receptor antagonist

Novel Inhibitor of the malaria parasite protein kinase CLK3, inhibiting the development of liver-stage parasites, killing asexual blood-stage parasites at the trophozoite and schizont stages of the erythrocytic cycle, blocking the development of sexual ga

Antimalarial; Novel inhibitor of HepG2

Potent TRPM8 antagonist, exhibiting antiallodynic properties in pain models

Non-competitive modulator of the proteasome inducing apoptosis a panel of myeloma and leukemia cell lines

Potent and selective antagonist of adenosine A2A receptors

Novel orally bioavailableγ-secretase modulator, reducing Aβ42 levels

Potent CB1 receptor inverse agonist

Aquaporin 1 (AQP1) channel blocker

Novel potent and selective ligand of Brd2(2)

Novel agonist for nicotinic acetylcholine receptors (nAChRs), modestly selectively targeting α6β2 subtype

Novel anti-angiogenesis and vascular disrupting agent, exhibiting moderate inhibitory cell proliferation activity

Novel anti-angiogenesis and vascular disrupting agent, exhibiting moderate inhibitory cell proliferation activity

Novel TBK1/IKKε inhibitor

Highly potent activator of Nrf2; Potent phase 2 cytoprotective pathway inducer and liver carcinogenesis blocker

Novel potent MCT1 inhibitor, exhibiting good single agent anticancer efficacy properties

Novel antibiotic against Mycobacterium tuberculosis (Mtb), potently killing replicating, virulent Mtb H37Rv in a clavulanate-dependent manner